These common heterocyclic compound, 546115-65-5, name is 1-(3-Bromophenyl)cyclopropanamine, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route. category: bromides-buliding-blocks
General procedure: 3-(trifluoromethyl)benzene-l-sulfonyl chloride (0.66 mL, 4.1 mmol) was added into a mixture of (3-bromophenyl)methanamine hydrochloride (1.0 g, 4.5 mmol) and DIEA(1.6 mL, 9.0 mmol) in DCM (20 mL). The reaction was stirred at room temperature for approximately 3 hours and washed with IN HC1 (IX) and brine (2X). The organic layer was dried over sodium sulfate, filtered, and concentrated in vacuo. The residue was purified by silica gel chromatography (0 – 30% EtOAc/Hexanes) to afford the title compound (1.5 g, 96%). l NMR (CDC13) delta 8.05 (s, IH), 8.00 (d, IH), 7.82 (d, IH), 7.63 (t, IH), 7.35 (m, IH), 7.27 (s, IH), 7.12 (d, 2H), 5.25 (t, IH), 4.18 (d, 2H).
The synthetic route of 1-(3-Bromophenyl)cyclopropanamine has been constantly updated, and we look forward to future research findings.
Reference:
Patent; VENENUM BIODESIGN LLC; HUANG, Chia-Yu; SHI, Dongchuan; KULTGEN, Steven G.; MCGUINNESS, Brian F; LETOURNEAU, Jeffrey J.; COLE, Andrew G.; BEASLEY, James R.; (358 pag.)WO2018/5801; (2018); A2;,
Bromide – Wikipedia,
bromide – Wiktionary